7月 2019 博客文章 (12,227)

Proteasome Inhibitors, Refined

The Proteasome is quite the structure. It is the shredding unit of the cell, where no-longer-needed proteins go to be ripped down to their components for recycling, and it’s become a more and more important part of drug discovery over the years. For one thing, all this fashionable targeted protein degradation work is about sending designated proteins off for destruction at will and…

MG132 (133407-82-6) Description:

MG132 is a specific, potent, reversible, and cell-permeable proteasome inhibitor (Ki = 4 nM) . It reduces the degradation of ubiquitin-conjugated proteins in mammalian cells and permeable strains of yeast by the 26S complex without affecting its ATPase or isopeptidase activities. MG132 activates c-Jun N-terminal kinase (JNK1), which initiates apoptosis. MG132 also inhibits NF-κB activation with…

(S)-MG132 is a reversible

MG132 is a reversible, cell-permeable inhibitor of proteasome activity (IC₅₀ = 100 nM; Kisselev & Goldberg) and calpain (IC₅₀ = 1.2 µM; Tsubuki et al.). The ubiquitin-proteasome pathway selectively degrades intracellular proteins, thereby clearing damaged or misfolded proteins, and regulating the availability of key proteins involved in the control of inflammatory processes and cell cycle…

MG132

133407-82-6 is a potent cell-permeable inhibitor of proteasome and calpain with IC50 of 100 nM and 1.2 μM respectively. MG132 inhibited the growth of HeLa cells via inducing the cell cycle arrest as well as triggering apoptosis. MG132 also inhibits NF-κB activation with an IC50 of 3 µM and prevents β-secretase cleavage. MG132 induces cell apoptosis through formation of reactive oxygen species or the upregulation and…

Grapiprant

In vitro, Grapiprant inhibits [(3)H">PGE(2) binding to both human and rat EP(4) receptors with K(i) of 13 +/- 4 and 20 +/- 1 nM, respectively. Grapiprant is highly selective for the human EP(4) receptor over other human prostanoid receptor subtypes. Grapiprant also inhibits PGE(2)-evoked elevation in intracellular cAMP at the human and rat EP(4) receptors with pA(2) of 8.3 +/- 0.03 and 8.2 +/- 0.2 nM,…